Becoming More Aware: March is National Caffeine Awareness Month

By Lorinda Sorensen, ND
Caffeine is a mild stimulant and is often quoted as the most widely used psychoactive drug in the world. Many people consume caffeine to increase alertness, help with memory, learning capacity and to gain pain relief. While there are people who can use caffeine-containing substances, especially coffee, on a daily basis without problems, high levels of caffeine intake can contribute to many physiological changes. Examples include an increase the sympathetic response, which can increase circulating catecholamine levels. This is primarily due to central antagonistic actions at adenosine receptors that ultimately regulate the paraventricular nucleus of the hypothalamus, which in turn influences the pituitary-adrenocortical (HPA) system. As a result of high caffeine intake, cortisol becomes elevated, too. Caffeine may also have another influence with hormones with some individuals having an increased steroidogenic acute regulatory protein (StAR) expression. [1]

Caffeine has a half-life that can range from 4 to 10 hours. In extremely high doses or overdose, the half-life may be as long as 15 hours. Some individuals with polymorphisms CYP1A2 isoenzyme, and pregnant women may have a prolonged clearance (slow metabolizers). Tobacco smoking accelerates caffeine metabolism and possibly smoking cannabis as well.

Caffeine-containing herbs include the well-known Coffee (Coffea species), the various forms of tea (Camillia sinensis) and the often desired Chocolate (Theobroma cocao). But don’t overlook Kola nut (Cola nitida or C. acuminata), Yerba Mate (Ilex paraguariensis) and Guarana (Paullinia cupana).

While coffee is often thought of as the main source for caffeine in the US, it does contain chlorogenic acid, the 2nd highest constituent after caffeine, and one of the most consumed polyphenols in the US diet. Chlorogenic acid may be one of the reasons that recent studies have shown coffee to be beneficial to prevent the onset of T2DM. Chlorogenic acid activates the adenosine monophosphate-activated protein kinase (AMPK) pathway, considered a main regulator of metabolism and a primary target for the treatment of T2DM.

Another constituent of coffee is the alkaloid trigonelline, a compound significantly responsible for coffee’s bitter taste and aroma. It is found in higher amount in Coffea arabica beans. The combination of trigonelline and chlorogenic acid, has been studied in humans to reduce insulin responses during an OGTT.[2]  Trigonelline has also been described as a phytoestrogen.[3]

For those clinicians and patients who are looking for caffeine-free options for hot beverages there are several herbal options. Tulsi or Holy Basil teas are available at many health food stores and come in various herbal combinations for different flavors. The traditional herbal teas of the southern Africa region are very popular. Rooibos or red bush tea (Aspalathus linearis) and Honeybush tea (Cyclopia intermedia) are both from the Fabaceae or legume family. Rooibios has significant antioxidant activity and has been described as a “mixture of honey, woody, and herbal-floral flavors with a slightly sweet taste and a subtle astringent mouthfeel.”[4]  Honeybush tea has a range of phytoestrogens including formononetin and coumestans as well as antioxidant polyphenols. [5],[6] For those who want to flavor of coffee or tea without the caffeine, supercritical CO2 extracts are becoming more available. This would be a good way to get the benefits of the various forms of tea (Camellia sinensis) without chemical residues.

Enjoyable as many caffeine products are, clinicians and patients should evaluate usage in terms in the endocrine system, discuss pros and cons of specific forms and the amount consumed to find alternatives or limit use if needed.

[1] Ping J, Lei YY, Liu L, Wang TT, Feng YH, Wang H. Inheritable stimulatory effects of caffeine on steroidogenic acute regulatory protein expression and cortisol production in human adrenocortical cells. Chem Biol Interact. 2012 Jan 5;195(1):68-75. doi: 10.1016/j.cbi.2011.11.001. Epub 2011 Nov 12. PubMed PMID: 22100783.
[2] van Dijk AE, Olthof MR, Meeuse JC, Seebus E, Heine RJ, van Dam RM. Acute effects of decaffeinated coffee and the major coffee components chlorogenic acid and trigonelline on glucose tolerance. Diabetes Care. 2009 Jun;32(6):1023-5. doi:10.2337/dc09-0207. Epub 2009 Mar 26. PubMed PMID: 19324944; PubMed Central PMCID: PMC2681030.
[3] Allred KF, Yackley KM, Vanamala J, Allred CD. Trigonelline is a novel phytoestrogen in coffee beans. J Nutr. 2009 Oct;139(10):1833-8. doi:10.3945/jn.109.108001. Epub 2009 Aug 26. PubMed PMID: 19710155.
[4] R. A. Street and G. Prinsloo, “Commercially Important Medicinal Plants of South Africa: A Review,” Journal of Chemistry, vol. 2013, Article ID 205048, 16 pages, 2013. doi:10.1155/2013/205048
[5] Louw A, Joubert E, Visser K. Phytoestrogenic potential of Cyclopia extracts and polyphenols. Planta Med. 2013 May;79(7):580-90. doi: 10.1055/s-0032-1328463.  Epub 2013 Apr 22. Review. PubMed PMID: 23609108.
[6] Verhoog, N.J.D., Joubert, E., Louw, A., 2007a. Screening of four Cyclopia (honeybush) species for putative phyto-oestrogenic activity by oestrogen receptor binding assays. South African Journal of Science 103, 13–21.

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